Dispiro 1,2,4-trioxolane antimalarials

Details Dispiro 1,2,4-trioxolane antimalarials Dispiro 1,2,4-trioxolane antimalarials

2007-10-31

2011-11-29

O Dell, David K (Department: 1625)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C514S462000, C549S337000, C544S006000, C544S148000, C544S374000, C540S543000, C546S015000

Reexamination Certificate

active

08067620

ABSTRACT:
A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the invention unexpectedly provide a single-dose cure for malaria, as well as prophylactic activity against the same. The compounds are also active against schistosomiasis and cancer.

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